- Title
- Isolation and characterisation of a channel inhibitor from Bunodosoma capense
- Creator
- Van Losenoord, Wynand
- Subject
- Bioactive compounds
- Subject
- Potassium channels Medical microbiology
- Date Issued
- 2019
- Date
- 2019
- Type
- Thesis
- Type
- Masters
- Type
- MSc
- Identifier
- http://hdl.handle.net/10948/44134
- Identifier
- vital:37114
- Description
- Voltage gated ion channels have recently become a subject of investigation as possible pharmaceutical targets. Research has linked the activity of ion channels directly to antiinflammatory pathways, energy homeostasis, cancer proliferation and painful diabetic neuropathy. Sea anemones secrete a diverse array of bioactive compounds including potassium and sodium channel inhibitors. A novel sodium channel inhibitor (molecular mass of 4619.7 ± 0.6 Da) with a predicted sequence: CLCNSDGPSV RGNTLSGILW LAGCPSGWHN CKKHKPTIGW CCK was isolated from Bunodosoma capense using a modified stimulation technique to induce the secretion of the neurotoxin rich mucus confirmed by an Artemia nauplii swimming assay. The peptide purification combined size-exclusion and reverse-phase high performance liquid chromatography. A thallium-based ion flux assay confirmed the presence of a sodium channel inhibitor and purity was determined using a modified tricine SDS-PAGE system. The peptide isolated indicated a tight conformation with the presence of multiple disulfide bonds in a cystine knot conformation. An IC50 value of 26 nM was determined for sodium channel inhibition on MCF-7 cells, indicating increased toxicity in comparison to sodium channel inhibitors previously isolated from Bunodosoma species.
- Format
- xvi, 129 leaves
- Format
- Publisher
- Nelson Mandela University
- Publisher
- Faculty of Science
- Language
- English
- Rights
- Nelson Mandela University
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NMU School of BioMolecular and Chemical Sciences
| Thumbnail | File | Description | Size | Format | |||
|---|---|---|---|---|---|---|---|
| View Details Download | SOURCE1 | Wynand van Losenoord.pdf | 10 MB | Adobe Acrobat PDF | View Details Download |